Introduction

Epigenetic changes such as DNA methylation and histone methylation and acetylation alter gene expression at the level of transcription by upregulating, downregulating, or silencing genes completely. Dysregulation of epigenetic events can be pathological, leading to cardiovascular disease, neurological disorders, metabolic disorders, and cancer development. Therefore, identifying drugs that inhibit these epigenetic changes are of great clinical interest. In our database we have the major classes of epigenetic drugs currently in use, such as DNA methylation inhibiting drugs, bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, protein methyltransferase inhibitors, and histone methylation inhibitors.

Source: Use of Epigenetic Drugs in Disease: An Overview, Sarah Heerboth et al.,2016


Proteins binding to methylated histones are involved in transcription regulation by allowing or disallowing access to target sites on histones. This is a novel class of epigenetic modifiers.

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Types of: PMHi
Drug Name FDA status
UNC669
UNC1215
Experimental
Experimental